PMID

Data

Article Title

Organization

Protective effect of novel substituted nicotine hydrazide analogues against hypoxic brain injury in neonatal rats via inhibition of caspase.

The Fifth Affiliated Hospital Of Guangzhou Medical University

Design, synthesis, and structure-activity relationships of novel benzothiazole derivatives bearing the ortho-hydroxy N-carbamoylhydrazone moiety as potent antitumor agents.

Key Laboratory Of Structure-Based Drug Design And Discovery (Shenyang Pharmaceutical University) Ministry Of Education

In vitro induction of apoptosis by isosclerone from marine-derived fungus Aspergillus fumigatus.

Pukyong National University

Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.

TBA

Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis.

Westf£Lische Wilhelms-Universit£T M£Nster

1,2-benzisothiazol-3-one derivatives as a novel class of small-molecule caspase-3 inhibitors.

Tianjin University Of Science And Technology

Influence of 4- or 5-substituents on the pyrrolidine ring of 5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin derivatives on their inhibitory activities towards caspases-3 and -7.

Westf£Lische Wilhelms-Universit£T M£Nster

Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.

Nankai University

Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography.

Westf£Lische Wilhelms-Universit£T M£Nster

Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: nonradioactive counterparts of putative PET-compatible apoptosis imaging agents.

Westf£Lische Wilhelms-Universit£T M£Nster

Irreversible inhibitors of cysteine proteases.

Dart Neuroscience

New description of protein-ligand interactions using a spherical self-organizing map.

Chugai Pharmaceutical

Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease.

Evotec (Uk)

A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.

Southern Medical University

Caspase-1 and -3 inhibiting drimane sesquiterpenoids from the extremophilic fungus Penicillium solitum.

University Of Montana

Isatin 1,2,3-triazoles as potent inhibitors against caspase-3.

University Of Oslo

Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.

University Of Florida

Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter And Gamble Pharmaceuticals

Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.

Procter & Gamble Pharmaceuticals

Fragment-based drug discovery.

Sunesis Pharmaceuticals

Protease inhibitors: current status and future prospects.

University Of Queensland

Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.

Maxim Pharmaceuticals

Peptidyl beta-homo-aspartals: specific inhibitors of interleukin-1 beta converting enzyme and its homologues (caspases).

Institute For Drug Research

Exploiting differences in caspase-2 and -3 S2 subsites for selectivity: structure-based design, solid-phase synthesis and in vitro activity of novel substrate-based caspase-2 inhibitors.

Chdi Management

Aspartic vinyl sulfones: inhibitors of a caspase-3-dependent pathway.

University Of Lisbon

Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.

Washington University

Synthesis and evaluation of vinyl sulfones as caspase-3 inhibitors. A structure-activity study.

University Of Lisbon

Turning enzymes ON with small molecules.

University Of California

Mechanisms, biology and inhibitors of deubiquitinating enzymes.

Institute For Bio-Medical Research

Design, synthesis, and discovery of novel non-peptide inhibitor of Caspase-3 using ligand based and structure based virtual screening approach.

Osmania University College For Women

Fluorinated isatin derivatives. Part 2. New N-substituted 5-pyrrolidinylsulfonyl isatins as potential tools for molecular imaging of caspases in apoptosis.

Westfalische Wilhelms-Universitat

Fluorinated isatin derivatives. Part 1: synthesis of new N-substituted (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatins as potent caspase-3 and -7 inhibitors.

WestfäLische Wilhelms-UniversitäT

Design, synthesis, and biological characterization of a caspase 3/7 selective isatin labeled with 2-[18F]fluoroethylazide.

Imperial College

Structure-based discovery of a novel non-peptidic small molecular inhibitor of caspase-3.

Tokyo University Of Science

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.

Epicept

Isatin sulfonamide analogs containing a Michael addition acceptor: a new class of caspase 3/7 inhibitors.

Washington University

Solid-phase analogue synthesis of caspase-3 inhibitors via palladium-catalyzed amination of 3-bromopyrazinones.

Merck Frosst Centre For Therapeutic Research

Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.

University Of Edinburgh

5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.

University Hospital Of The WestfäLische Wilhelms-UniversitäT

Synthesis and evaluation of unsaturated caprolactams as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter & Gamble Pharmaceuticals

Synthesis, radiolabeling, and in vivo evaluation of an 18F-labeled isatin analog for imaging caspase-3 activation in apoptosis.

Washington University

Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.

Procter & Gamble Pharmaceuticals

Discovery and Crystallographic Studies of Nonpeptidic Piperazine Derivatives as Covalent SARS-CoV-2 Main Protease Inhibitors.

Shandong University

Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.

Procter & Gamble Pharmaceuticals

Discovery and structure-activity relationship of 3-aryl-5-aryl-1,2,4-oxadiazoles as a new series of apoptosis inducers and potential anticancer agents.

Maxim Pharmaceuticals

Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme.

Procter & Gamble Pharmaceuticals

Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.

Merck Research Laboratories

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P2 alpha-amino acid by a alpha-hydroxy acid.

Maxim Pharmaceuticals

Discovery and Crystallographic Studies of Trisubstituted Piperazine Derivatives as Non-Covalent SARS-CoV-2 Main Protease Inhibitors with High Target Specificity and Low Toxicity.

Shandong University

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.

Merck Frosst Centre For Therapeutic Research

Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.

University Of Illinois At Chicago

Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1.

Pfizer

Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: SAR of the N-protecting group.

Maxim Pharmaceuticals

Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke.

Idun Pharmaceuticals

Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis.

Galapagos

Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.

Idun Pharmaceuticals

Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization.

Idun Pharmaceuticals

Acyl dipeptides as reversible caspase inhibitors. Part 1: initial lead optimization.

Idun Pharmaceuticals

Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.

Merck Research Laboratories

Optimization of the

Novartis Pharma

Fragment Linking Strategies for Structure-Based Drug Design.

Universit£

Quinolone hybrids and their anti-cancer activities: An overview.

Qilu University Of Technology (Shandong Academy Of Sciences)

Discovery of Fluoromethylketone-Based Peptidomimetics as Covalent ATG4B (Autophagin-1) Inhibitors.

Roche Pharma Research And Early Development

Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.

Basf Bioresearch

Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines.

Hebei University Of Science & Technology

Conformationally constrained inhibitors of caspase-1 (interleukin-1 beta converting enzyme) and of the human CED-3 homologue caspase-3 (CPP32, apopain).

Idun Pharmaceuticals

Development of a potent and selective cell penetrant Legumain inhibitor.

Queen'S University Belfast

Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.

Harbor Branch Oceanographic Institution

Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.

Harbor Branch Oceanographic Institution

Structure-activity relationship study of a series of caspase inhibitors containing ?-amino acid moiety for treatment of cholestatic liver disease.

Wuxi Apptec (Shanghai)

Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.

Nestl�

Chemical Approaches to Intervening in Ubiquitin Specific Protease 7 (USP7) Function for Oncology and Immune Oncology Therapies.

Progenra

Blockade of Asparagine Endopeptidase Inhibits Cancer Metastasis.

Emory Chemical Biology Discovery Center Emory University School Of Medicine Atlanta

Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.

The University Of Arizona

Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors.

University Of Colorado

Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke.

Taisho Pharmaceutical

Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy.

University Of Illinois

3,4-Dihydropyrimido(1,2-a)indol-10(2H)-ones as potent non-peptidic inhibitors of caspase-3.

Wyeth Research

Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.

Washington University

Biochemical and biophysical characterization of inhibitor binding to caspase-3 reveals induced asymmetry.

Wyeth Research

Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.

Merck Frosst Canada

Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.

Merck Research Laboratories

Nicotinyl aspartyl ketones as inhibitors of caspase-3.

Merck Frosst Canada

Lipophilic versus hydrogen-bonding effect in P3 on potency and selectivity of valine aspartyl ketones as caspase 3 inhibitors.

Merck Frosst Canada

1,3-Dioxo-4-methyl-2,3-dihydro-1H-pyrrolo[3,4-c]quinolines as potent caspase-3 inhibitors.

Chemical Diversity Research Institute

Synthesis and structure-activity relationship of 4-substituted 2-(2-acetyloxyethyl)-8-(morpholine-4-sulfonyl)pyrrolo[3,4-c]quinoline-1,3-diones as potent caspase-3 inhibitors.

Chemical Diversity Research Institute

N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies.

Washington University

Potent and selective nonpeptide inhibitors of caspases 3 and 7.

Glaxosmithkline

Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors.

Shanghai Institutes For Biological Sciences

Discovery of a novel class of reversible non-peptide caspase inhibitors via a structure-based approach.

Burnham Institute

Identification of potent and novel small-molecule inhibitors of caspase-3.

Sunesis Pharmaceuticals

Inhibition of human caspases by peptide-based and macromolecular inhibitors.

Merck Research Laboratories

Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.

Sunesis Pharmaceuticals